Lomerizine hydrochloride

Lomerizine hydrochloride was introduced as Teranas and Migsis in Japan for the treatment of migraine. It is the first in its class of dual sodium and calcium channel blockers to be marketed for this indication. It can be synthetically obtained by reductive amination of 2,3,4-trimethoxybenzaldehyde with the appropiate benzhydryl piperazine. In dogs, Lomerizine exerts a potent, selective and long-lasting vasodilation of cerebral arteries related to a combination of mechanisms, especially a functional block of L-type voltagesensitive calcium channels (L-VSCCs). Lomerizine increases cerebral blood flow compared to peripheral blood flow with only weak effects on systemic arterial blood pressure. Other mechanisms involved could be blockade of other VSCC and sodium channels, 5-HT2 and alpha-1 receptors. As a reducing agent of cortical spreading depression and neurogenic inflammation, Lomerizine was shown to be useful in migraine. In an open clinical study, it demonstrated efficacy in the treatment of cluster headache. Moreover, it may have utility in other neurological diseases such as cerebrovascular ischemia or cerebral infarction.

Colourless Crystalline Solid

Akzo Nobel (Netherlands)

A diphenylpiperazine calcium channel blocker. A selective cerebral vasodilator. Antimigraine.

Teranas;Migsis

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[4] DONNA L. SAVIGNI . Three Ca2+ channel inhibitors in combination limit chronic secondary degeneration following neurotrauma[J]. Neuropharmacology, 2013, 75: Pages 380-390. DOI:10.1016/j.neuropharm.2013.07.034
[5] LUAN T. TRAN. The voltage-gated calcium channel blocker lomerizine is neuroprotective in motor neurons expressing mutant SOD1, but not TDP-43[J]. Journal of Neurochemistry, 2014, 130 3: 455-466. DOI:10.1111/jnc.12738
[6] RYAN L. O’HARE DOIG . Specific combinations of ion channel inhibitors reduce excessive Ca2+ influx as a consequence of oxidative stress and increase neuronal and glial cell viability in vitro[J]. Neuroscience, 2016, 339: Pages 450-462. DOI:10.1016/j.neuroscience.2016.10.005